Medicinal compounds
AssigneeGlaxo Group Limited
InventorsKeith Biggadike, Philip Box, Diane Coe, Duncan Holmes, Brian Looker, Panayiotis Procopiou
Life of this patent
Estimating the term…
Abstract
A compound of formula (I) or a salt, solvate, or physiologically functional derivative thereof, wherein: m is an integer of from 2 to 8; n is an integer of from 2 to 5; with the proviso that m+n is 4 to 10; R4 and R5 are independently selected from hydrogen and C1-4alkyl with the proviso that the total number of carbon atoms in R4 and R5 is not more than 4; R6 and R7 are independently selected from hydrogen and C1-4alkyl with the proviso that the total number of carbon atoms in R6 and R7 is not more than 4, and Ar1 is a group selected from (a), (b), (c) and (d).
Claims42
A compound of formula (I)
- or a salt, solvate, or physiologically functional derivative thereof, wherein:
- m is an integer of from 2 to 8;
- n is an integer of from 2 to 5;
- with the proviso that m+n is 4 to 10;
- R1 is selected from hydrogen, C1-6alkyl, hydroxy, halo, C1-6haloalkyl, —CN, —XC(O)NR9R10, —XNR8C(O)R9, —XNR8C(O)NR9R10, —XNR8SO2R9, —XSO2NR9R10, XNR8SO2NR9R10,
- -XNR9R10, XN+R8R9R10, —XNR8C(O)OR9, —XCO2R9, —XNR8C(O)NR8C(O)NR9R10, —XSR9, XSOR9, and —XSO2R9;
- or R1 is selected from —X-aryl, —X-hetaryl, and —X-(aryloxy), each optionally substituted by 1 or 2 groups independently selected from hydroxy, C1-6alkoxy, halo, C1-6alkyl,
- C1-6haloalkyl, —NHC(O)(C1-6alkyl), —SO2(C1-6alkyl), —SO2(aryl), —SO2NH2, —SO2N H(1-6alkyl), —SO2N H(C3-7cycloalkyl), —CO2H, —CO2(C1-6-alkyl), —SO2NH(C3-7cycloalkylC1-6alkyl), —NH2, —NH(C1-6alkyl), or hetaryl optionally substituted by 1 or 2 groups independently selected from hydroxy, C1-6alkoxy, halo, C1-6alkyl, or
- C1-6haloalkyl;
- X is —(CH2)p— or C2-6 alkenylene;
- p is an integer from 0 to 6;
- R8 and R9 are independently selected from hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, hetaryl, hetaryl(C1-6alkyl)- and aryl(C1-6alkyl)- and R8 and R9 are each independently optionally substituted by 1 or 2 groups independently selected from halo, C1-6alkyl,
- C1-6haloalkyl, —NHC(O)(C1-6alkyl), —SO2(C1-6alkyl), —SO2(aryl), —CO2H, —CO2(C1-4alkyl),
- —NH2, —NH(C1-6alkyl), aryl(C1-6alkyl)-, aryl(C2-6alkenyl)-, aryl(C2-6alkynyl)-, hetaryl(C1-6alkyl)-, —NHSO2aryl, —NH(hetarylC1-6alkyl), —NHSO2hetaryl, —NHSO2(C1-6alkyl), —NHC(O)aryl, or —NHC(O)hetaryl:
- or when R1 is —XNR8C(O)NR9R10, R8 and R9 may, together with the —NC(O)N-portion of the group R1 to which they are bonded, form a saturated or unsaturated ring;
- or where R1 is —XNR8C(O)OR9, R8 and R9 may, together with the —NC(O)O-portion of the group R1 to which they are bonded, form a saturated or unsaturated ring;
- R10 is selected from hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, hetaryl, hetaryl(C1-6alkyl)- and aryl(C1-6alkyl)-, or R9 and R10, together with the nitrogen to which they are bonded, form a 5-, 6-, or 7-membered nitrogen containing ring;
- and R9 and R10 are each optionally substituted by one or two groups independently selected from halo, C1-6alkyl, and C1-6haloalkyl;
- R2 is selected from hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, halo, aryl, aryl(C1-6alkyl)-, C1-6haloalkoxy, and C1-6 haloalkyl;
- R3 is selected from hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, halo, aryl, aryl(1-6alkyl)-, C1-6haloalkoxy, and C1-6haloalkyl;
- R4 and R5 are independently selected from hydrogen and C1-4 alkyl with the proviso that the total number of carbon atoms in R4 and R5 is not more than 4;
- R6 and R7 are independently selected from hydrogen and C1-4alkyl with the proviso that the total number of carbon atoms in R6 and R7 is not more than 4, and
- Ar1 is a group selected from
- wherein R11 represents hydrogen, halogen, —(CH2)qOR15, —NR15C(O)R16, —NR15SO2R16,
- —SO2NR15R16, —NR15R16, —OC(O)R17 or OC(O)NR15R16,
- and R12 represents hydrogen, halogen or C1-4 alkyl;
- or R11 and R12 together with the benzene ring atoms to which they are attached form a 5- or 6-membered heterocyclic ring;
- R13 represents hydrogen, halogen, —OR15 or —NR15R16;
- R14 represents hydrogen, halogen, haloC1-4 alkyl, —OR15, —NR15R16, —OC(O)R17 or OC(O)NR15R16;
- R15 and R16 each independently represents hydrogen or C1-4 alkyl, or in the groups —NR15R16, —SO2NR15R16 and —OC(O)NR15R16, R15 and R16 independently represent hydrogen or C1-4 alkyl or together with the nitrogen atom to which they are attached form a 5-, 6- or 7-membered nitrogen-containing ring,
- R17 represents an aryl group which may be unsubstituted or substituted by one or more substituents selected from halogen, C1-4 alkyl,
- hydroxy, C1-4 alkoxy or halo C1-4 alkyl;
- and
- q is zero or an integer from 1 to 4,
- provided that in the group (a) when R11 represents —(CH2)qOR15 and q is 1, R13 is not OH.
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Dependencies are inferred from the claim text.